1359431-16-5
1359431-16-5 structure
- Name: M435-1279
- Chemical Name: M435-1279
- CAS Number: 1359431-16-5
- Molecular Formula: C18H17N3O5S2
- Molecular Weight: 419.47
- Catalog: Signaling Pathways Metabolic Enzyme/Protease E1/E2/E3 Enzyme
- Create Date: 2022-01-11 13:20:58
- Modify Date: 2024-01-09 19:11:18
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M435-1279 is a UBE2T inhibitor. M435-1279 acts inhibit the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1[1].
| Name | M435-1279 |
|---|
| Description | M435-1279 is a UBE2T inhibitor. M435-1279 acts inhibit the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1[1]. |
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| Related Catalog | |
| Target |
UBE2T |
| In Vitro | M435-1279 (0, 2, 4, 8, 16, 31 μM; 48 h) significantly inhibits the growth of HGC27, AGS, and MKN45 cells[1]. M435-1279 (0, 4, 8, 12, 16, 20 μM) inhibits the cell viability whit a IC50 s of 16.8, 11.88, 6.93, 7.76 μM of GES-1, HGC27, MKN45, AGS cells, respectively[1]. M435-1279 (31 nM to 500 μM) binding to UBE2T whit a KD value of 50.5 μM[1]. M435-1279 has high LD50 (15.6 g/kg), LOAEL (0.207g/kg), and has a EC50 value of 7.47mg/L[1]. M435-1279 (11.88 μM; 48 h) inhibits the ubiquitination of RACK1 and the hyperactivation of the Wnt/β-catenin pathway[1]. Cell Viability Assay[1] Cell Line: HGC27, AGS, and MKN45 cells Concentration: 0, 2, 4, 8, 16, 31 μM Incubation Time: 48 h Result: Inhibited the cell growth. Cell Viability Assay[1] Cell Line: HGC27, AGS, and MKN45 cells Concentration: 0, 4, 8, 12, 16, 20 μM Incubation Time: Result: Inhibited the cell viability whit a IC50s of 16.8, 11.88, 6.93, 7.76 μM in GES-1, HGC27, MKN45, AGS cells, respectively. |
| In Vivo | M435-1279 (5 mg/kg/day; intratumor injections for 18 days) slows the tumor growth. M435-1279 induces higher RACK1 proteins expression, and lower Ki-67 and β-catenin proteins expression in intratumor tumors[1]. Animal Model: BALB/C nude mice CDX model (MKN45 tumor size: 75–100 mm3) [1] Dosage: 5 mg/kg/day Administration: intratumor injections for 18 days Result: Slowed the tumor growth. Induced higher RACK1 proteins expression, and lower Ki-67 and β-catenin proteins expression in intratumor tumors. |
| References |
| Molecular Formula | C18H17N3O5S2 |
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| Molecular Weight | 419.47 |
| Hazard Codes | Xi |
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